Drug intelligence / Profile preview

bendamustine dodecyl ester

Development stage
Phase 1
Lead developer
Roche
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

RXDX-107 is a nanoparticle-based formulation containing the alkyl (dodecanol) ester of bendamustine, a bifunctional mechlorethamine derivative and alkylating agent. The drug is encapsulated in human serum albumin (HSA) nanoparticles to improve pharmacokinetics, including increased half-life and enhanced tumor tissue biodistribution. Upon administration, RXDX-107 allows for high concentrations of the active compound at tumor sites. The mechanism of action involves DNA alkylation and crosslinking by the released bendamustine derivative, leading to inhibition of DNA, RNA, and protein synthesis and ultimately inducing apoptosis in cancer cells. Preclinical studies have demonstrated anti-tumor activity across multiple solid tumor models including breast, lung, ovarian cancer as well as non-small cell lung cancer (NSCLC). RXDX-107 was developed to address limitations of standard bendamustine in solid tumors due to its short half-life[1][2][3][5][6].

Other names
bendamustine-containing nanoparticle-based formulation RXDX-107bendamustine dodecyl ester
02

Targets

DNA

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